Design and Optimization of 3′-(Imidazo[1,2-a]pyrazin-3-yl)-[1,1′-biphenyl]-3-carboxamides as Selective DDR1 Inhibitors

Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors

The structure-based design of 1, 2, 3, 4-tetrahydroisoquinoline derivatives as selective DDR1 inhibitors is reported. One of the representative compounds, 6j, binds to DDR1 with a Kd value of 4.7 nM and suppresses its kinase activity with an IC50 value of 9.4 nM, but it is significantly less potent for a panel of 400 nonmutated kinases. 6j also demonstrated reasonable pharmacokinetic properties...

Synthesis and in-vitro antimicrobial screening of 3-cinnamoyl coumarin and 3-[3-(1H-indol-2-yl)-3-aryl-propanoyl]-2H-chromen-2-ones

An efficient synthesis of some novel coumarin derivatives via 1, 4- Michael addition of indole to coumarin chalcones catalyzed by cellulose sulphonic acid (CSA) under solvent free conditions is described. The corresponding Michael addition products were obtained in good to excellent yield. The synthesized compounds were screened for their antibacterial activity against E. coli, S. aureus and an...

Synthesis and in-vitro antimicrobial screening of 3-cinnamoyl coumarin and 3-[3-(1H-indol-2-yl)-3-aryl-propanoyl]-2H-chromen-2-ones

An efficient synthesis of some novel coumarin derivatives via 1, 4- Michael addition of indole to coumarin chalcones catalyzed by cellulose sulphonic acid (CSA) under solvent free conditions is described. The corresponding Michael addition products were obtained in good to excellent yield. The synthesized compounds were screened for their antibacterial activity against E. coli, S. aureus and an...

Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors.

Novel benzofuran-2-carboxamide ligands, which are selective for sigma receptors, have been synthesized via a microwave-assisted Perkin rearrangement reaction and a modified Finkelstein halogen-exchange used to facilitate N-alkylation. The ligands synthesized are the 3-methyl-N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides (KSCM-1, KSCM-5 and KSCM-11). The benzofuran-2-carboxamide...

design, synthesis, and evaluation of 3-(benzylpyridinium-4-yl-methylene) oxindole derivatives as ache inhibitos